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Pharmacology

Chapter 11

QuestionAnswer
When should the dental health care provider asses the pt.'s anxiety? On both first and subsequent visits.
Why will the health care provider use orally administered drugs to provide relaxation for an anxious pt. and not use (IV) administration? Most states require separate certificates for (IV) or conscious sedation.
In the largest dose given of Sedative-Hypnotic Agents, what is produced? General anesthesia and death.
What level of the Sedative-Hypnotic Agents, produce the anxiolytic effect? Small dose
What agents can produce varying degree of the CNS depression, depending on the dose administered? Sedative-Hypnotic Agents
What do small doses of Sedative-Hypnotic Agents produce? CNS depression (sedation), reduction of activity, and simple anxiety.
What do the large doses of Sedative-Hypnotic Agents do? Produce CNS depression in greater amounts.
T/F Benzodizapines are named according to their reactions. False-the structures are what combines them together in a group.
What two Benzodiapines were named in Dr. Dawson's lecture? Chlordiazepoxide (Librium) and Diazepam (Valium)
In what forms are Benzodizapines available? Tablets, capsules, oral solutions, rectal gel, and injectable form.
When Benzodizapines are administered by the oral route they are well absorbed and the onset of action is related to their lipid solubility. First is true, second is false; both are true; both are false; first is false, second is true Both are true
What route of Benzodizapines are administered that produce a rapid and predictable response that is ideal for conscious sedation? IV administration
What does the Benzodizapines cross to produce an effect on the CNS and the fetus? Blood-brain barrier and placental barriers
Benzodizapines enhance or facilitate the action of what neurotransmitter, that is a major inhibitory transmitter in the CNS? GABA y-aminobutyric acid, the inhibitor is enhanced
T/F The clinical effects in humans are anxiety and panic reduction at low doses and drowsiness and even sleep at higher doses belong to the Antiseizure Effects section. F- Behavioral effects; Antiseizure effects increase the seizure threshold.
Muscle Relaxation can produce relaxation of what? Skeletal Muscle
In general Benzodizapines are what? Used alone, have a wide margin of safety, similar adverse effects, but differ in their frequency.
What are the most common side effects of Benzodizapines? A. CNS depression B. Fatigue C. Drowsiness D. Muscle weakness E.Ataxia F. GI Effects G. All the above H. A-E H. A-E
The use of parenteral Benzodizapines during the dental appointment reduces and alters what? Anxiety and alters perception of time.
What drug has a long half-life and metabolizes to an active metabolite to prolong its duration? Diazepam
What drug is metabolized primarily to inactivate metabolites? Midazolam (Versed)
This drug is found in Europe primarily but is sold into the US illegally and used inappropriately (been secretly given to women who were then ________). Fill in the blank. What am I? Date Rape, Flunitrazepam (Rohypnol)
Anterograde Amnesia produces what? Amnesia at the beginning, when the drug is taken.
What effect does Dizapam have on an outpatient dental procedure? Respiratory depression
Some cardiovascular effects may do what what a relief of anxiety occurs? Fall in blood pressure and plus rate
What visual effects are contraindicated and produced when taking Benzodiazepines? Angle-closure (narrow-angle) glaucoma, diplopia ( single object viewed as two), nystagmus (rythmic oscillation of the eyeballs), and blurred vision.
When taking Benzodiazapines, what are the common dental effects that are produced? Xerostomia, increased salivation, swollen tongue, and a bitter metallic taste.
Thrombophelbitis is what? Extreme irritation of the veins
Why may Parenteral Diazepam cause thrombophelbitis? Propylene glycol is used to solubilize it.
Benzodiazepines will interact in a "________" fashion with other CNS depressants. additive
T/F: Selective serotonin uptake inhibitors do not alter the clearance of diazepam. False- they do alter the clearance of diazepam
Levodopa's effectiveness is reduced by, A. Diazepam B. Levodopa C. Benzodiazepines D. Barbiturates C. Benzodiazepines
Barbiturates increase the effect of digoxin, phenytonin, and probenecide. Benzodiazepines are useful in short-term treatment of anxiety, panic attacks, insomnia, and alcohol withdrawal. A. both are true B. both are false C. first is false second is true C. first is true second is false
"_______" is used for acute treatment of seizures and conscious sedation as well as "_______" or during surgery. Benzodiazepines and general anesthesia
What are the manifestations of anxiety? Restlessness, tension, tachycardia, and dyspena
Medical uses for Benzodiazepine include what, A. anxiety control B. insomnia management C. treatment of epilepsy (seizures) D. all the above D. all the above
What are the two drugs of choice for an emergency situation in the treatment of epilepsy( seizures), A. digoxin B. diazepam C. probenecid D. lorazepam B. diazepam and D. lorazepam
What is the purpose of Benzodiazepines in combination (treatment) of alcohol? Used to treat alcohol withdrawal syndrome
What is the treatment to control muscle spasms (multiple sclerosis and cerebral palsy)? Benzodiazepines
What does orally administered diazepam do for dental procedures? allay apprehension
When is premedication used and why? before surgical procedures to allay anxiety
Conscious sedation with benzodiazepines is usually accompanied by what? IV administration
What two forms of amnesia can develop with conscious sedation accompanied by IV administration? Anterograde amnesia and Retrograde amnesia
What is it called when you forget the events after the injections? Anterograde amnesia
What is retrograde amnesia? Take the pill and forget what has happened before you took the pill
What type of benzodiazepines have been associated with respiratory depression and arrest when used for conscious sedation? Parenteral Benzodiazepines
What requires continuous monitoring of respiratory and cardiac functions and requires a dentist to have additional training? conscious sedation
What three benzodiazepines agents are most common according to Dr. Dawson in lecture? A. alprazolam (xanax) B. diazepam (valium) C. midazolam (versed) D. flurazepam (Dalmane) E. all the above A-C
"_______" are the original sedative-hypnotic agents? barbiturates
What is one noted good thing about barbiturates and one bad thing? problems with their use are well documented and are associated with a high rate of abuse and complete cardiovascular and respiratory depression with an over-dose
What drug has almost completely replaced the barbiturates for treating anxiety and insomia? A. methohexital B. secobarbital C. benzodiasepines D. amobarbital C. benzodiazepines
Barbiturates are still used at "_______" and to "_____,______,_______". anticonvulsants, induce general anesthesia
How are barbiturates absorbed and used? orally and rectally; intravenously but not intramuscular
IV agents that are inactivated by redistribution from site of action in the CNS, to muscles and adipose tissue. This belongs to what pharmacokinetics of barbiturates? distribution
"______" barbiturates are rapidly and almost completely metabolized by the liver. Short and intermediate- acting
Where are long-acting barbiturates excreted and how? kidneys as a free drug
How do barbiturates produce their effect? Enhance GABA receptor binding and prolonging the opening of chloride channels
Why may barbiturates act directly on chloride channels? if you are given higher doses of barbiturates
Mechanism of barbiturates may account for what? ability to induce surgical anesthesia and pronounced generalized CNS depression effects.
What is the main pharmacological effect of barbiturates? CNS depression
What occurs with a normal dose of barbiturates? relaxation
What occurs with an intermediate dose of barbiturates? inhibitory fibers of the CNS are depressed, resulting in dis-inhibition and euphoria
What occurs with a high dose of barbiturates? hypnosis can be produced
What occurs with the max dose of barbiturates? anesthesia with respiratory and cardiovascular depression and finally arrest
T/F: Barbiturates have a significant analgesic effect F-they don't have a significant analgesic effect
Barbiturates have an anti-convulsant action. Long-acting agents are used to treat epilepsy. A. both are true B. both are false C. first is true, second is false D. first is false, second is true A. both are true
Sedatives do not provide "_____". analgesia
When should these drugs never be administered unless it may benefit them more than it would be a risk? pregnant women due to risking the fetus
What may be attempted when taking sedative-hypnotic drugs? suicide
"_______" and "______" dependence has been observed with almost all drugs used to allay anxiety. psychic and physical
T/F: Depression caused by all sedative-hypnotics will add to depression caused by other CNS depressants. True-an additive of depression does occur
What are the uses for centrally acting muscle relaxants? adjunct to rest and physical therapy for relief of muscle spasms associated with acute painful musculoskeletal conditions. May be used for symptomatic relief of TMJ disorder
What drugs are examples of centrally acting skeletal muscle relaxants? carisoprodol (Soma); chlorzoxazone (Parafon Forte DSC); methocarbamol (Robaxin); orphenadrine (Norflex); cyclobenzapine (Flexeril); diazepam (Valium)
What does baclofen (Lioresal) do? inhibits both monosynaptic and polysynaptic reflexes at the spinal level
What is baclofen (Lioresal) indicated for? spasticity from multiple scerosis or spinal cord injuries or diseases
Both sedation and analgesia can be obtained from what? opioid analgesics
A nonopioid or an opioid can be used concomitantly with a sedative in what case? when anxiety is an important component in pain relief
What statements are special considerations to remember? Pt.'s who are to use antianxiety agents should be driven to and from the dental appointment. Drugs are not a substitute for pt. management
An indenofuran derivative is highly selective for what? melatonin type 1 (MT1) and melatonin type 2 (MT2) receptors
MT1 receptors may mediate phase-shifting effects of melatonin on a 24-hour biologic clock while MT 2 receptor regulates sleep: a. both are true b. both are false c. first is true, 2nd is false d. first is false, 2nd is true both are false-MT1 receptors regulate sleep while MT2 receptors mediate phase-shifting effects of melatonin on a 24-hour biologic clock
Centrally acting muscle relaxants do what? exert their effects on the CNS to produce skeletal muscle relaxation
What statements correlate with the pharmacologic effects of centrally acting muscle relaxants? all CNS relaxants produce some degree of sedative effect because their action is on the CNS. The sedative effects dominate over the "selective" muscle-relaxant activity. Useful in treating uscle spasms and back and neck pain.
What statement belong to the overview of centrally acting muscle relaxants? exert their muscle-relaxing properties indirectly by producing CNS depression. Have no direct effect on striated muscle; do not directly relax tense skeletal muscles
Zolpidem (ambien) has hypnotic and anxiolytic effects but what does the receptor specificity produce? less muscle relaxant and anticonvulsant effects.
What are likely to be useful in dentistry when an oral anxiolytic agent is desired for relaxing an anxious dentalpatient? zolpidem (Ambien)
T/F: Zolpidem (Ambien ) is a rapid-acting hypnotic that is less potent and has a shorter duration of action than buspirone (BuSpar). F- Zaleplon (Sonata) is a rapid-action hypnotic that is less potent and has a shorter duration of action than zolpidem
What drug appears to have a lower risk of next day risidual effects, even with use in middle of the night? zaleplon (Sonata)
This drug is known for anterograde amnesia, an unpleasant taste, and impaired driving the morning after nighttime administration eszopiclone (Lunesta)
What is an melatonin receptor agonist that has been approved for treatment of insomnia characterized by diffulculty falling asleep? ramelteon (Rozeram)
Whose mechanism of action is unknown and believed to be related to interactions with neurotransmitters in the CNS? buspirone (BuSpar)
Why are buspirone (BuSpar) anxioselective? due to its selective anxiolytic action without hypnotic, anticonvulsant, or muscle-relaxant properties
What do most pt.'s pefer? Benzodiazepines
What three drugs comprise a new class of drugs that are not benzodiasepines but appear to bind to benzodiazepine receptors and decrease sleep latency with little effect on sleep stages? zolpidem, zaleplon, and eszopidone
What drugs are all thought to have agonist effects on GABA? a. zolpidem b. buspirone (buspar) c. benzodiasepines d. zaleplon e. eszopidone f. all the above all the above: zolpidem, buspirone (buspar), benzodiasepines, zaleplon, eszopidone
T/F: zolpidem, zaleplon, and eszopidone are used to treat epilepsy only. F-zolpidem, zaleplon, and eszopidone are used to treat insomnia only
What is zolpidem (ambien) recently developed hypnotic used for? short-term management of insomnia
What are therapeutic uses determined by? duration of action
What type of barbiturates are used intravenously for induction of general anesthesia? ultra-short acting barbiturates
What type of barbiturates have little medical use and are replaced by benzodiasepines? short- and intermediate-acting barbiturates
Long-acting barbiturates are used for what? treatment of epiepsy
What is another name for the nonbenzodiazepine- nonbarbiturate sedative-hypnotics? chloral hydrate (noctec) "mickey-finn" and buspirone (buspar)
What statement belongs to chloral hydrate (noctec)? an inexpensive, orally effective sedative-hypnotic drug with a rapid onset and short duration of action
Therapeutic doses of chloral hydrate (norcet) do not produce what? pronounced respiratory or cardiovascular depression
What is used in dentistry for preoperative sedation for children and at what dose? chloral hydrate (noctec); 50 mh/kg up to maximum of 1g
T/F: a larger and larger dose must be used to produce an effect, and this dose can approximate the lethal dose true-dose to produce an effect can result in the lethal dose
What is porphyria? a group of disorders involving heme biosynthesis
Barbiturates are recommended with porphyria. They are recommended with intermittent or a positive family history of porphyria: a. both are true b. both are false c. 1st is true, 2nd is false d. 1st is false, 2nd is true both are false- barbiturates contraindicated in both pt.'s with porphyria
Why are barbiturates contraindicated in pt.'s with porphyria? they stimulate an increase the synthesis of porphyrins which are already at an excessive level in this disease
Barbiturates are simulators of what? liver microsomal enzyme production
What are liver microsomal enzymes responsible for metabolism? many drugs
an increase in the liver microsomal enzymes could do what? Increase the rate of drug destruction and decrease duration of action
With a usual dose barbiturates are relatively safe. CNS depression may be exaggerated in debilitated pt. or those with liver or kidney impairment: a. both are true b. both are false c. 1st is true 2nd is false d. first is false second is true both are true
what is an important fact with anesthetic dose? with higher doses, concentrations in the blood can be lethal
What statement does acute poisoning belong with? lethal dose can only be approximated, severe poisoning will follow ingestion of 10x the hypnotic dose; life may be threatened when more than 15x the hypnotic dose is consumed
chronic use of barbiturates can lead to what dependence? physical and psycological
how does an addict act over barbiturates? progressively depressed and is unable to function
T/F: tolerance develops to most effects and the lethal dose? F- tolerance does develop to most effects but not to the lethal dose
Created by: daisenmurray